General Information of Target

Target ID LDTP00938
Target Name NUAK family SNF1-like kinase 1 (NUAK1)
Gene Name NUAK1
Gene ID 9891
Synonyms
ARK5; KIAA0537; OMPHK1; NUAK family SNF1-like kinase 1; EC 2.7.11.1; AMPK-related protein kinase 5; ARK5; Omphalocele kinase 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEGAAAPVAGDRPDLGLGAPGSPREAVAGATAALEPRKPHGVKRHHHKHNLKHRYELQET
LGKGTYGKVKRATERFSGRVVAIKSIRKDKIKDEQDMVHIRREIEIMSSLNHPHIISIYE
VFENKDKIVIIMEYASKGELYDYISERRRLSERETRHFFRQIVSAVHYCHKNGVVHRDLK
LENILLDDNCNIKIADFGLSNLYQKDKFLQTFCGSPLYASPEIVNGRPYRGPEVDSWALG
VLLYTLVYGTMPFDGFDHKNLIRQISSGEYREPTQPSDARGLIRWMLMVNPDRRATIEDI
ANHWWVNWGYKSSVCDCDALHDSESPLLARIIDWHHRSTGLQADTEAKMKGLAKPTTSEV
MLERQRSLKKSKKENDFAQSGQDAVPESPSKLSSKRPKGILKKRSNSEHRSHSTGFIEGV
VGPALPSTFKMEQDLCRTGVLLPSSPEAEVPGKLSPKQSATMPKKGILKKTQQRESGYYS
SPERSESSELLDSNDVMGSSIPSPSPPDPARVTSHSLSCRRKGILKHSSKYSAGTMDPAL
VSPEMPTLESLSEPGVPAEGLSRSYSRPSSVISDDSVLSSDSFDLLDLQENRPARQRIRS
CVSAENFLQIQDFEGLQNRPRPQYLKRYRNRLADSSFSLLTDMDDVTQVYKQALEICSKL
N
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CAMK Ser/Thr protein kinase family, SNF1 subfamily
Subcellular location
Nucleus
Function
Serine/threonine-protein kinase involved in various processes such as cell adhesion, regulation of cell ploidy and senescence, cell proliferation and tumor progression. Phosphorylates ATM, CASP6, LATS1, PPP1R12A and p53/TP53. Acts as a regulator of cellular senescence and cellular ploidy by mediating phosphorylation of 'Ser-464' of LATS1, thereby controlling its stability. Controls cell adhesion by regulating activity of the myosin protein phosphatase 1 (PP1) complex. Acts by mediating phosphorylation of PPP1R12A subunit of myosin PP1: phosphorylated PPP1R12A then interacts with 14-3-3, leading to reduced dephosphorylation of myosin MLC2 by myosin PP1. May be involved in DNA damage response: phosphorylates p53/TP53 at 'Ser-15' and 'Ser-392' and is recruited to the CDKN1A/WAF1 promoter to participate in transcription activation by p53/TP53. May also act as a tumor malignancy-associated factor by promoting tumor invasion and metastasis under regulation and phosphorylation by AKT1. Suppresses Fas-induced apoptosis by mediating phosphorylation of CASP6, thereby suppressing the activation of the caspase and the subsequent cleavage of CFLAR. Regulates UV radiation-induced DNA damage response mediated by CDKN1A. In association with STK11, phosphorylates CDKN1A in response to UV radiation and contributes to its degradation which is necessary for optimal DNA repair.
TTD ID
T21653
Uniprot ID
O60285
DrugMap ID
TT65FL0
Ensemble ID
ENST00000261402.7
HGNC ID
HGNC:14311
ChEMBL ID
CHEMBL5784

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
DU145 SNV: p.Y55H .
HCT15 SNV: p.D644E .
HT3 SNV: p.S325F .
IPC298 SNV: p.W305Ter .
Ishikawa (Heraklio) 02 ER SNV: p.P463S .
LN18 Deletion: p.Q617_Y628del .
LNCaP clone FGC SNV: p.G281V .
MCC26 Substitution: p.P506L .
MELJUSO SNV: p.R599L .
MEWO SNV: p.E272K .
NCIH23 SNV: p.E346Ter .
RKO SNV: p.I91T .
RL SNV: p.H40R; p.S312G .
TE10 SNV: p.E324D .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C519(1.28)  LDD3338  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0369  CL100 HEK-293T C519(0.94)  LDD1573  [2]
 LDCM0373  CL104 HEK-293T C519(0.90)  LDD1577  [2]
 LDCM0377  CL108 HEK-293T C519(1.05)  LDD1581  [2]
 LDCM0382  CL112 HEK-293T C519(0.87)  LDD1586  [2]
 LDCM0386  CL116 HEK-293T C519(1.16)  LDD1590  [2]
 LDCM0391  CL120 HEK-293T C519(0.98)  LDD1595  [2]
 LDCM0395  CL124 HEK-293T C519(0.99)  LDD1599  [2]
 LDCM0399  CL128 HEK-293T C519(0.98)  LDD1603  [2]
 LDCM0403  CL16 HEK-293T C519(0.92)  LDD1607  [2]
 LDCM0416  CL28 HEK-293T C519(1.08)  LDD1620  [2]
 LDCM0429  CL4 HEK-293T C519(1.21)  LDD1633  [2]
 LDCM0430  CL40 HEK-293T C519(1.13)  LDD1634  [2]
 LDCM0443  CL52 HEK-293T C519(0.92)  LDD1646  [2]
 LDCM0456  CL64 HEK-293T C519(0.94)  LDD1659  [2]
 LDCM0469  CL76 HEK-293T C519(1.17)  LDD1672  [2]
 LDCM0482  CL88 HEK-293T C519(0.87)  LDD1685  [2]
 LDCM0022  KB02 EFO-21 C519(2.45)  LDD2321  [1]
 LDCM0023  KB03 EFO-21 C519(2.08)  LDD2738  [1]
 LDCM0024  KB05 MV4-11 C519(1.28)  LDD3338  [1]

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402